丙型肝炎病毒NS5B聚合酶变构抑制剂BMS-961955的发现。
Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase.
作者信息
Zheng Barbara Zhizhen, D'Andrea Stanley V, Hanumegowda Umesh, Knipe Jay O, Mosure Kathy, Zhuo Xiaoliang, Lemm Julie A, Liu Mengping, Rigat Karen L, Wang Ying-Kai, Fang Hua, Poronsky Chris, Cutrone Jingfang, Wu Dauh-Rurng, Arunachalam Pirama Nayagam, Balapragalathan T J, Arumugam Arunachalam, Mathur Arvind, Meanwell Nicholas A, Gao Min, Roberts Susan B, Kadow John F
机构信息
Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
Department of Discovery Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.
出版信息
Bioorg Med Chem Lett. 2017 Aug 1;27(15):3294-3300. doi: 10.1016/j.bmcl.2017.06.024. Epub 2017 Jun 11.
The synthesis, structure-activity relationship (SAR) data, and further optimization of the metabolic stability and pharmacokinetic (PK) properties for a previously disclosed class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors are described. These efforts led to the discovery of BMS-961955 as a viable contingency backup to beclabuvir which was recently approved in Japan for the treatment of HCV as part of a three drug, single pill combination marketed as Ximency.
本文描述了一类先前公开的环丙基稠合吲哚并苯并氮杂卓丙肝病毒NS5B聚合酶抑制剂的合成、构效关系（SAR）数据，以及对其代谢稳定性和药代动力学（PK）性质的进一步优化。这些研究工作促成了BMS-961955的发现，它可作为beclabuvir的备用药物，beclabuvir最近在日本被批准用于治疗丙肝，作为一种名为Ximency的三药单片复方制剂的一部分。
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